DEVELOPMENT OF A PARENTERALLY ADMINISTRABLE HYDROSOL PREPARATION OF THE 3RD-GENERATION PLATINUM COMPLEX [(+ -FLUOROPHENYL)ETHYLENEDIAMINE]DICHLOROPLATINUM(II) .1. PREPARATION AND STUDIES ON THE STABILITY AND ANTITUMOR-ACTIVITY/

The development of a galenical formulation for poorly water soluble di chloroplatinum(II) complexes suitable for the parenteral administratio n in cancer chemotherapy is described. The procedure, which we elabora ted for 4-fluorophenyl)ethlenediamine]dichloroplatinum(II) (rac-4F-PtC l2), is based on the reaction of a soluble diaquaplatinum(II) salt wit h sodium chloride in water in the presence of pluronic F 68 as stabili zer and results in a sufficiently stable colloidal solution (i.e. hydr osol). In contrast to the poorly water soluble synthetic rac-4F-PtCl2, which was ineffective towards the hormone sensitive MXT-M-3.2 breast cancer of the mouse, its hydros of formulation proved to be highly act ive and was very well tolerated.